PE20020332A1 - DERIVATIVES OF 4-PHENYL-PYRIDINE AS ANTAGONISTS OF NEUROQUININ NK-1 RECEPTORS - Google Patents

DERIVATIVES OF 4-PHENYL-PYRIDINE AS ANTAGONISTS OF NEUROQUININ NK-1 RECEPTORS

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Publication number
PE20020332A1
PE20020332A1 PE2001000779A PE2001000779A PE20020332A1 PE 20020332 A1 PE20020332 A1 PE 20020332A1 PE 2001000779 A PE2001000779 A PE 2001000779A PE 2001000779 A PE2001000779 A PE 2001000779A PE 20020332 A1 PE20020332 A1 PE 20020332A1
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Peru
Prior art keywords
halogen
alkyl
trifluoromethyl
alcoxy
neuroquinin
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PE2001000779A
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Spanish (es)
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Thierry Godel
Torsten Hoffmann
Patrick Schnider
Heinz Stadler
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Hoffmann La Roche
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Publication of PE20020332A1 publication Critical patent/PE20020332A1/en

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Abstract

SE REFIERE A DERIVADOS DE 4-FENIL PIRIDINA DE FORMULA I DONDE R ES H, HALOGENO, R1 ES (C=C)mR1', (CR'=CR")mR1'; R1 ES HALOGENO, CIANO, (C)mR'R"R5; CONR'R", COO(CH2)mR5, ENTRE OTROS; R' Y R" SON H, OH, ALQUILO, CICLOALQUILO, ARILO; R5 ES H, CIANO, OH, HALOGENO, TRIFLUOROMETILO, ENTRE OTROS; R6 ES H, ALQUILO, TRIFLUOROMETILO, ARILO, ENTRE OTROS; R7 ES CO(CH2)mOH, OXO; R2 ES H, ALQUILO, ALCOXI, HALOGENO, CF3; R3 Y R3' SON H, ALQUILO O FORMAN JUNTOS CICLOALQUILO; R4 Y R4' SON H, HALOGENO, CF3, ALQUILO, ALCOXI; R Y R2, R4 Y R4' SON HC=CH-CH=CH OPCIONALMENTE SUSTITUIDO POR ALQUILO HALOGENO, ALCOXI; X ES CONR8, (CH2)pO, NR8CO, ENTRE OTROS; n ES 1-2; m ES 0-4; o Y p SON 1-2. SON COMPUESTOS PREFERIDOS N-(3,5-BIS-TRIFLUOROMETIL-BENCIL)-6-(4-HIDROXIACETIL-PIPERACIN-1-ILO)-N-METIL-4-o-TOLIL-NICOTINAMIDA, N-(3,5-BIS-TRIFLUOROMETIL-BENCIL)-6-CLORO-N-METIL-4-o-TOLIL-NICOTINAMIDA, ENTRE OTROS; TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION. LOS COMPUESTOS SON ANTAGONISTAS DE RECEPTORES DE NEUROQUININA NK-1 Y PUEDEN SER UTILES PARA EL TRATAMIENTO DE ARTRITIS REUMATOIDE, ASMA, ENFERMEDAD INFLAMATORIA DEL INTESTINO, MODULACION DEL SISTEMA NERVIOSO CENTRALREFERS TO 4-PHENYL PYRIDINE DERIVATIVES OF FORMULA I WHERE R IS H, HALOGEN, R1 IS (C = C) mR1 ', (CR' = CR ") mR1 '; R1 IS HALOGEN, CYANE, (C) mR' R "R5; CONR'R ", COO (CH2) mR5, AMONG OTHERS; R 'AND R" ARE H, OH, ALKYL, CYCLOALKYL, ARYL; R5 IS H, CYANE, OH, HALOGEN, TRIFLUOROMETHYL, AMONG OTHERS; R6 IS H, ALKYL, TRIFLUOROMETHYL, ARYL, AMONG OTHERS; R7 IS CO (CH2) mOH, OXO; R2 IS H, ALKYL, ALCOXY, HALOGEN, CF3; R3 AND R3 'ARE H, ALKYL, OR TOGETHER FORM CYCLOALKYL; R4 AND R4 'ARE H, HALOGEN, CF3, ALKYL, ALCOXY; R AND R2, R4 AND R4 'ARE HC = CH-CH = CH OPTIONALLY SUBSTITUTED BY ALKYL HALOGEN, ALCOXY; X IS CONR8, (CH2) pO, NR8CO, AMONG OTHERS; n IS 1-2; m IS 0-4; o AND p ARE 1-2. PREFERRED COMPOUNDS ARE N- (3,5-BIS-TRIFLUOROMETHYL-BENZYL) -6- (4-HYDROXIACETIL-PIPERACIN-1-ILO) -N-METHYL-4-o-TOLIL-NICOTINAMIDE, N- (3,5- BIS-TRIFLUORomethyl-BENZYL) -6-CHLORO-N-METHYL-4-o-TOLYL-NICOTINAMIDE, AMONG OTHERS; IT ALSO REFERS TO A PROCEDURE FOR PREPARATION. THE COMPOUNDS ARE ANTAGONISTS OF NEUROQUININ NK-1 RECEPTORS AND MAY BE USEFUL FOR THE TREATMENT OF RHEUMATOID ARTHRITIS, ASTHMA, INFLAMMATORY DISEASE OF THE BOWEL, MODULATION OF THE CENTRAL NERVOUS SYSTEM

PE2001000779A 2000-08-08 2001-08-06 DERIVATIVES OF 4-PHENYL-PYRIDINE AS ANTAGONISTS OF NEUROQUININ NK-1 RECEPTORS PE20020332A1 (en)

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